Development of a chitosan based double layer-coated tablet as a platform for colon-specific drug delivery
Min Soo Kim,1,* Dong Woo Yeom,1,* Sung Rae Kim,1 Ho Yub Yoon,1 Chang Hyun Kim,1 Ho Yong Son,1 Jin Han Kim,1 Sangkil Lee,2 Young Wook Choi1 1College of Pharmacy, Chung-Ang University, Seoul, 2College of Pharmacy, Keimyung University, Daegu, South Korea *These authors contributed equally to this wor...
| Main Authors: | , , , , , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
Dove Medical Press
2016-12-01
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| Series: | Drug Design, Development and Therapy |
| Subjects: | |
| Online Access: | https://www.dovepress.com/development-of-a-chitosan-based-double-layer-coated-tablet-as-a-platfo-peer-reviewed-article-DDDT |
| _version_ | 1828328589373734912 |
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| author | Kim MS Yeom DW Kim SR Yoon HY Kim CH Son HY Kim JH Lee S Choi YW |
| author_facet | Kim MS Yeom DW Kim SR Yoon HY Kim CH Son HY Kim JH Lee S Choi YW |
| author_sort | Kim MS |
| collection | DOAJ |
| description | Min Soo Kim,1,* Dong Woo Yeom,1,* Sung Rae Kim,1 Ho Yub Yoon,1 Chang Hyun Kim,1 Ho Yong Son,1 Jin Han Kim,1 Sangkil Lee,2 Young Wook Choi1 1College of Pharmacy, Chung-Ang University, Seoul, 2College of Pharmacy, Keimyung University, Daegu, South Korea *These authors contributed equally to this work Abstract: A double layer-coated colon-specific drug delivery system (DL-CDDS) was developed, which consisted of chitosan (CTN) based polymeric subcoating of the core tablet containing citric acid for microclimate acidification, followed by an enteric coating. The polymeric composition ratio of Eudragit E100 and ethyl cellulose and amount of subcoating were optimized using a two-level factorial design method. Drug-release characteristics in terms of dissolution efficiency and controlled-release duration were evaluated in various dissolution media, such as simulated colonic fluid in the presence or absence of CTNase. Microflora activation and a stepwise mechanism for drug release were postulated. Consequently, the optimized DL-CDDS showed drug release in a controlled manner by inhibiting drug release in the stomach and intestine, but releasing the drug gradually in the colon (approximately 40% at 10 hours and 92% at 24 hours in CTNase-supplemented simulated colonic fluid), indicating its feasibility as a novel platform for CDD. Keywords: chitosan, colon-specific delivery, acidification, microflora, factorial design, controlled release |
| first_indexed | 2024-04-13T20:11:26Z |
| format | Article |
| id | doaj.art-111dd034df4240e5b41fb7c362de59e6 |
| institution | Directory Open Access Journal |
| issn | 1177-8881 |
| language | English |
| last_indexed | 2024-04-13T20:11:26Z |
| publishDate | 2016-12-01 |
| publisher | Dove Medical Press |
| record_format | Article |
| series | Drug Design, Development and Therapy |
| spelling | doaj.art-111dd034df4240e5b41fb7c362de59e62022-12-22T02:31:50ZengDove Medical PressDrug Design, Development and Therapy1177-88812016-12-01Volume11455730604Development of a chitosan based double layer-coated tablet as a platform for colon-specific drug deliveryKim MSYeom DWKim SRYoon HYKim CHSon HYKim JHLee SChoi YWMin Soo Kim,1,* Dong Woo Yeom,1,* Sung Rae Kim,1 Ho Yub Yoon,1 Chang Hyun Kim,1 Ho Yong Son,1 Jin Han Kim,1 Sangkil Lee,2 Young Wook Choi1 1College of Pharmacy, Chung-Ang University, Seoul, 2College of Pharmacy, Keimyung University, Daegu, South Korea *These authors contributed equally to this work Abstract: A double layer-coated colon-specific drug delivery system (DL-CDDS) was developed, which consisted of chitosan (CTN) based polymeric subcoating of the core tablet containing citric acid for microclimate acidification, followed by an enteric coating. The polymeric composition ratio of Eudragit E100 and ethyl cellulose and amount of subcoating were optimized using a two-level factorial design method. Drug-release characteristics in terms of dissolution efficiency and controlled-release duration were evaluated in various dissolution media, such as simulated colonic fluid in the presence or absence of CTNase. Microflora activation and a stepwise mechanism for drug release were postulated. Consequently, the optimized DL-CDDS showed drug release in a controlled manner by inhibiting drug release in the stomach and intestine, but releasing the drug gradually in the colon (approximately 40% at 10 hours and 92% at 24 hours in CTNase-supplemented simulated colonic fluid), indicating its feasibility as a novel platform for CDD. Keywords: chitosan, colon-specific delivery, acidification, microflora, factorial design, controlled releasehttps://www.dovepress.com/development-of-a-chitosan-based-double-layer-coated-tablet-as-a-platfo-peer-reviewed-article-DDDTChitosancolon-specific deliveryacidificationmicroflorafactorial designcontrolled release |
| spellingShingle | Kim MS Yeom DW Kim SR Yoon HY Kim CH Son HY Kim JH Lee S Choi YW Development of a chitosan based double layer-coated tablet as a platform for colon-specific drug delivery Drug Design, Development and Therapy Chitosan colon-specific delivery acidification microflora factorial design controlled release |
| title | Development of a chitosan based double layer-coated tablet as a platform for colon-specific drug delivery |
| title_full | Development of a chitosan based double layer-coated tablet as a platform for colon-specific drug delivery |
| title_fullStr | Development of a chitosan based double layer-coated tablet as a platform for colon-specific drug delivery |
| title_full_unstemmed | Development of a chitosan based double layer-coated tablet as a platform for colon-specific drug delivery |
| title_short | Development of a chitosan based double layer-coated tablet as a platform for colon-specific drug delivery |
| title_sort | development of a chitosan based double layer coated tablet as a platform for colon specific drug delivery |
| topic | Chitosan colon-specific delivery acidification microflora factorial design controlled release |
| url | https://www.dovepress.com/development-of-a-chitosan-based-double-layer-coated-tablet-as-a-platfo-peer-reviewed-article-DDDT |
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